Home MAPK Raf inhibitor Tovorafenib (MLN2480) For research use only.

Tovorafenib (MLN2480)

Synonyms: BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101

Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.

Tovorafenib (MLN2480) Chemical Structure

Tovorafenib (MLN2480) Chemical Structure

CAS No. 1096708-71-2

Purity & Quality Control

Tovorafenib (MLN2480) Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Tovorafenib (MLN2480, BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Targets
Raf [1]
In vitro
In vitro

MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo[1].

It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts[2].

In vitro analysis of this drug combination of MLN2480 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity .In addition, western blot analysis demonstrates the effect of MLN2480 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK[1][2].
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-ERK / ERK 28082416
In Vivo
In vivo

In vivo, MLN2480 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models[3].

MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects[2].
Animal Research Animal Models C57BL/6J mice
Dosages 12.5 mg/kg
Administration oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06381570 Recruiting
Low-grade Glioma
Daniel Morgenstern|The Hospital for Sick Children
 March 21 2024 Early Phase 1
NCT05566795 Recruiting
Low-grade Glioma
Day One Biopharmaceuticals Inc.|SIOPe Brain Tumor Group LOGGIC Consortium
 February 27 2023 Phase 3
NCT04985604 Recruiting
Melanoma|Solid Tumor|CRAF Gene Amplification|RAF1 Gene Amplification|BRAF Gene Fusion|BRAF Fusion|CRAF Gene Fusion|CRAF Fusion|RAF1 Gene Fusion|RAF1 Fusion|Thyroid Cancer Papillary|Spitzoid Melanoma|Pilocytic Astrocytoma|Pilocytic Astrocytoma Adult|Non Small Cell Lung Cancer|Non-Small Cell Adenocarcinoma|Colorectal Cancer|Pancreatic Acinar Carcinoma|Spitzoid Malignant Melanoma|Bladder Cancer|Bladder Urothelial Carcinoma|MAP Kinase Family Gene Mutation|RAS Mutation|RAF Mutation|MEK Mutation
Day One Biopharmaceuticals Inc.
 July 15 2021 Phase 1|Phase 2
NCT04775485 Recruiting
Low-grade Glioma|Advanced Solid Tumor
Day One Biopharmaceuticals Inc.|Pacific Pediatric Neuro-Oncology Consortium
 April 22 2021 Phase 2
NCT03429803 Active not recruiting
Low-grade Glioma
Karen D. Wright MD|PLGA Fund at Pediatric Brain Tumor Foundation|National Cancer Institute (NCI)|Pacific Pediatric Neuro-Oncology Consortium|Team Jack Foundation|Day One Biopharmaceuticals Inc.|Dana-Farber Cancer Institute
 February 27 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 506.29 Formula

C17H12Cl2F3N7O2S
CAS No. 1096708-71-2 SDF Download Tovorafenib (MLN2480) SDF
Smiles CC(C1=NC=C(S1)C(=O)NC2=NC=C(C(=C2)C(F)(F)F)Cl)NC(=O)C3=C(C(=NC=N3)N)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (197.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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